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Naslov:Comparative study of interactions of aliskiren and AT [sub] 1 receptor antagonists with lipid bilayers
Avtorji:ID Sadegphour, A. (Avtor)
ID Rappolt, Michael (Avtor)
ID Ntountaniotis, Dimitrios (Avtor)
ID Chatzigeorgioug, Petros (Avtor)
ID Viras, Kyriakos (Avtor)
ID Megariotis, Grigorios (Avtor)
ID Papadopoulos, M. (Avtor)
ID Siapi, Eleni (Avtor)
ID Mali, Gregor (Avtor)
ID Mavromoustakos, Thomas Michael (Avtor)
Datoteke:URL URL - Izvorni URL, za dostop obiščite https://www.sciencedirect.com/science/article/pii/S0005273614004325?via=ihub
 
Jezik:Angleški jezik
Tipologija:1.01 - Izvirni znanstveni članek
Organizacija:Logo KI - Kemijski inštitut
Povzetek:The renin-angiotensin-aldosterone system (RAAS) plays a key role in the regulation of blood pressure. Renin is the rate limiting enzyme of the RAAS and aliskiren is a highly potent and selective inhibitor of the human renin. Renin is known to be active both in the circulating blood stream as well as locally, when bound to the (pro)-renin receptor ((P)RR). In this study we have investigated a possible mechanism of action of aliskiren, in which its accumulation in the plasma membrane is considered as an essential step for effective inhibition. Aliskiren's interactions with model membranes (cholesterol rich and poor) have been investigated by applying different complementary techniques: differential scanning calorimetry (DSC), Raman spectroscopy, magic angle spinning (MAS) nuclear magnetic resonance (NMR) spectroscopy and small- and wide-angle X-ray scattering (SAXS and WAXS). In addition, in silico molecular dynamics (MD) calculations were applied for further confirmation of the experimental data. Aliskiren's thermal effects on the pre- and main transition of dipalmitoyl-phosphatidylcholine (DPPC) membranes as well as its topographical position in the bilayer show striking similarities to those of angiotens.in II type 1 receptor (AT1R) antagonists. Moreover, at higher cholesterol concentrations aliskiren gets expelled from the membrane just as it has been recently demonstrated for the angiotensin receptor blocker (ARB) losartan. Thus, we propose that both the AT1R and the (P)RR-bound renin active sites can be efficiently blocked by membrane-bound ARBs and aliskiren when cholesterol rich membrane rafts/caveolae are formed in the vicinity of the receptors.
Ključne besede:aliskiren, renin, PRR, DPPC bilayers, raman spectroscopy, solid state NMR spectroscopy, SAXS and WAXS, MD simulations
Status publikacije:Objavljeno
Leto izida:2015
Št. strani:str. 984-994
Številčenje:Vol. 1848, iss. 4
PID:20.500.12556/DiRROS-765 Novo okno
UDK:577.2
ISSN pri članku:0005-2736
DOI:10.1016/j.bbamem.2014.12.004 Novo okno
COBISS.SI-ID:5618202 Novo okno
Opomba:Sodelavci: M. Rappolt, D. Ntountaniotis, P. Chatzigeorgiou, K. Viras, G. Megariotis, M. G. Papadopoulos, E. Siapi, G. Mali, and T. Mavromoustakos;
Datum objave v DiRROS:26.01.2015
Število ogledov:5045
Število prenosov:506
Metapodatki:XML DC-XML DC-RDF
:
SADEGPHOUR, A., RAPPOLT, Michael, NTOUNTANIOTIS, Dimitrios, CHATZIGEORGIOUG, Petros, VIRAS, Kyriakos, MEGARIOTIS, Grigorios, PAPADOPOULOS, M., SIAPI, Eleni, MALI, Gregor in MAVROMOUSTAKOS, Thomas Michael, 2015, Comparative study of interactions of aliskiren and AT [sub] 1 receptor antagonists with lipid bilayers. Biochimica et biophysica acta [na spletu]. 2015. Vol. 1848, no. 4, p. 984–994. [Dostopano 12 april 2025]. DOI 10.1016/j.bbamem.2014.12.004. Pridobljeno s: https://www.sciencedirect.com/science/article/pii/S0005273614004325?via=ihub
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Gradivo je del revije

Naslov:Biochimica et biophysica acta
Skrajšan naslov:Biochim. biophys. acta, Biomembr.
Založnik:Elsevier
ISSN:0005-2736
COBISS.SI-ID:4077101 Novo okno

Sekundarni jezik

Jezik:Ni določen
Ključne besede:zgradba molekule, receptorji, lipidi


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